CN103446088A - Application of Incarviatone A in skin cancer treatment drug - Google Patents
Application of Incarviatone A in skin cancer treatment drug Download PDFInfo
- Publication number
- CN103446088A CN103446088A CN2013104321825A CN201310432182A CN103446088A CN 103446088 A CN103446088 A CN 103446088A CN 2013104321825 A CN2013104321825 A CN 2013104321825A CN 201310432182 A CN201310432182 A CN 201310432182A CN 103446088 A CN103446088 A CN 103446088A
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- Prior art keywords
- incarviatone
- skin cancer
- application
- preparation
- cancer treatment
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
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- 201000000849 skin cancer Diseases 0.000 title claims abstract description 19
- 239000003814 drug Substances 0.000 title claims abstract description 16
- 208000000453 Skin Neoplasms Diseases 0.000 title abstract description 8
- 229940079593 drug Drugs 0.000 title abstract description 7
- 150000001875 compounds Chemical class 0.000 claims description 17
- 201000008261 skin carcinoma Diseases 0.000 claims description 11
- 238000002360 preparation method Methods 0.000 abstract description 12
- 102100027833 14-3-3 protein sigma Human genes 0.000 abstract description 6
- 101100107350 Homo sapiens SFN gene Proteins 0.000 abstract description 6
- 230000002401 inhibitory effect Effects 0.000 abstract description 4
- 230000000259 anti-tumor effect Effects 0.000 abstract description 2
- 238000011161 development Methods 0.000 abstract description 2
- 238000011156 evaluation Methods 0.000 abstract description 2
- AZKSAVLVSZKNRD-UHFFFAOYSA-M 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide Chemical compound [Br-].S1C(C)=C(C)N=C1[N+]1=NC(C=2C=CC=CC=2)=NN1C1=CC=CC=C1 AZKSAVLVSZKNRD-UHFFFAOYSA-M 0.000 abstract 2
- 239000003560 cancer drug Substances 0.000 abstract 1
- 230000000459 effect on growth Effects 0.000 abstract 1
- 238000000338 in vitro Methods 0.000 abstract 1
- 230000012010 growth Effects 0.000 description 6
- 230000000694 effects Effects 0.000 description 4
- 229930014626 natural product Natural products 0.000 description 4
- IAZDPXIOMUYVGZ-UHFFFAOYSA-N Dimethylsulphoxide Chemical compound CS(C)=O IAZDPXIOMUYVGZ-UHFFFAOYSA-N 0.000 description 3
- 239000002246 antineoplastic agent Substances 0.000 description 3
- 229940041181 antineoplastic drug Drugs 0.000 description 3
- 239000001963 growth medium Substances 0.000 description 3
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 description 2
- 241001121991 Incarvillea delavayi Species 0.000 description 2
- 206010028980 Neoplasm Diseases 0.000 description 2
- 239000002671 adjuvant Substances 0.000 description 2
- 201000011510 cancer Diseases 0.000 description 2
- 239000002775 capsule Substances 0.000 description 2
- 230000005764 inhibitory process Effects 0.000 description 2
- 230000031700 light absorption Effects 0.000 description 2
- 239000000203 mixture Substances 0.000 description 2
- 238000001228 spectrum Methods 0.000 description 2
- 230000004083 survival effect Effects 0.000 description 2
- 241001597008 Nomeidae Species 0.000 description 1
- 229930012538 Paclitaxel Natural products 0.000 description 1
- 229920002472 Starch Polymers 0.000 description 1
- 230000001464 adherent effect Effects 0.000 description 1
- 230000001093 anti-cancer Effects 0.000 description 1
- 238000003556 assay Methods 0.000 description 1
- 238000004113 cell culture Methods 0.000 description 1
- 230000010261 cell growth Effects 0.000 description 1
- 239000012531 culture fluid Substances 0.000 description 1
- 201000010099 disease Diseases 0.000 description 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 1
- 238000002474 experimental method Methods 0.000 description 1
- 231100000206 health hazard Toxicity 0.000 description 1
- 150000002611 lead compounds Chemical class 0.000 description 1
- 238000000034 method Methods 0.000 description 1
- 238000011275 oncology therapy Methods 0.000 description 1
- 229960001592 paclitaxel Drugs 0.000 description 1
- 230000003285 pharmacodynamic effect Effects 0.000 description 1
- 238000012545 processing Methods 0.000 description 1
- 239000000047 product Substances 0.000 description 1
- 238000012827 research and development Methods 0.000 description 1
- 235000019698 starch Nutrition 0.000 description 1
- 239000008107 starch Substances 0.000 description 1
- 239000006228 supernatant Substances 0.000 description 1
- RCINICONZNJXQF-MZXODVADSA-N taxol Chemical compound O([C@@H]1[C@@]2(C[C@@H](C(C)=C(C2(C)C)[C@H](C([C@]2(C)[C@@H](O)C[C@H]3OC[C@]3([C@H]21)OC(C)=O)=O)OC(=O)C)OC(=O)[C@H](O)[C@@H](NC(=O)C=1C=CC=CC=1)C=1C=CC=CC=1)O)C(=O)C1=CC=CC=C1 RCINICONZNJXQF-MZXODVADSA-N 0.000 description 1
- 238000012360 testing method Methods 0.000 description 1
Landscapes
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
The invention discloses application of Incarviatone A in preparation of a skin cancer treatment drug and belongs to the technical field of novel medicine application. Evaluation of in-vitro thiazolyl blue (MTT) anti-tumor activity shows that the Incarviatone A also has remarkable inhabiting effect on growth of human skin cancer cell strains A431, HME1, A375 and SK23. Therefore, the Incarviatone A can be used for preparation of an anti-skin cancer drug and has good development and application prospect. The application of the Incarviatone A in the preparation of the skin cancer treatment drug is disclosed for the first time. Due to the fact that the fact that the skeleton type is a novel skeleton type, and the high skin cancer cell inhibiting activity of the Incarviatone A is previously unimagined.
Description
Technical field
The present invention relates to the new purposes of Compound I ncarviatone A, relate in particular to the application of Incarviatone A in the anti-skin carcinoma medicine of preparation.
Technical background
Cancer is to one of disease of human life's health hazard maximum, and annual have a large amount of people to die from cancer.The research and development of cancer therapy drug are the focuses of study of pharmacy always.In antitumor drug, have 74% to be the natural product or derivatives thereof, as paclitaxel and derivant thereof are exactly the reasonable antitumor drug of effect clinically at present.Therefore, from natural product, searching anticancer compound or lead compound have great importance.
The Compound I ncarviatone A the present invention relates to is one and within 2012, delivers (Shen, Y.H.et al., 2012.Incarviatone A, a structurally unique natural product hybrid with a new carbon skeleton from Incarvillea delavayi, and its absolute configuration via calculated electronic circular dichroic spectra.RSC Advances2, 4175 – 4180.) New skeleton compound, this compound has brand-new framework types, there is no at present the report about this compound activity aspect, purposes for the Incarviatone A the present invention relates in preparation treatment skin carcinoma medicine belongs to open first, because framework types belongs to brand-new framework types, and its inhibition for skin cancer cell is active unexpectedly strong, there do not is the possibility that is provided any enlightenment by other compounds, possesses outstanding substantive distinguishing features, control for skin carcinoma simultaneously obviously has significant progress.
Summary of the invention
The invention provides the application of Compound I ncarviatone A in preparing antitumor drug.
The present invention adopts following technical scheme: the application of Incarviatone A in the anti-skin carcinoma medicine of preparation, and the structural formula of Incarviatone A is as shown in formula I:
The present invention finds by external MTT anti-tumor activity evaluation, and Incarviatone A also has significant inhibitory action to the growth of application on human skin JEG-3 A431, HME1, A375 and SK23, suppresses the IC of this 4 strain Growth of Cells
50value is respectively 1.23 ± 0.13 μ M, 2.24 ± 0.17 μ M, 1.21 ± 0.21 μ M and 2.10 ± 0.18 μ M.Therefore, Incarviatone A can, for the preparation of anti-skin carcinoma medicine, have good development prospect.
The purposes of the Incarviatone A the present invention relates in preparation treatment skin carcinoma medicine belongs to open first, because framework types belongs to brand-new framework types, and its inhibition for skin cancer cell is active unexpectedly strong, there do not is the possibility that is provided any enlightenment by other compounds, possess outstanding substantive distinguishing features, the control for skin carcinoma simultaneously obviously has significant progress.
The present invention is further detailed explanation by the following examples, but protection scope of the present invention is not subject to any restriction of specific embodiment, but be limited by claim.
The specific embodiment
The preparation method of Compound I ncarviatone A involved in the present invention is referring to document (Shen, Y.H.et al., 2012.Incarviatone A, a structurally unique natural product hybrid with a new carbon skeleton from Incarvillea delavayi, and its absolute configuration via calculated electronic circular dichroic spectra.RSC Advances2,4175 – 4180.).
The present invention is further detailed explanation by the following examples, but protection scope of the present invention is not subject to any restriction of specific embodiment, but be limited by claim.
Embodiment 1: the preparation of Compound I ncarviatone A tablet involved in the present invention:
Get 20 and digest compound Incarviatone A, add conventional adjuvant 180 grams that prepare tablet, mix, conventional tablet machine is made 1000.
Embodiment 2: the preparation of Compound I ncarviatone A capsule involved in the present invention:
Get 20 and digest compound Incarviatone A, add the conventional adjuvant for preparing capsule as starch 180 grams, mix, encapsulatedly make 1000.
Further illustrate its pharmaceutically active below by pharmacodynamic experiment.
Experimental example: adopt the growth inhibited effect of mtt assay assessing compound Incarviatone A to the application on human skin JEG-3
1. method: in the cell of growth logarithmic (log) phase: application on human skin JEG-3 A431, HME1, A375 and SK23(buy from Chinese Academy of Sciences's cell bank) with 1.5 * 10
4the concentration kind is in 96 orifice plates.Suck original culture medium after cell culture 24h is adherent.Test is divided into blank group, drug treating group.Blank group is changed 1640 culture medium containing 10% hyclone; It is 100 μ M that the drug treating group is changed containing concentration, 50 μ M, 10 μ M, 1 μ M, 0.1 μ M, the culture medium of the Incarviatone A of 0.01 μ M and 0.001 μ M.After cultivating 48h, add the MTT of concentration 5mg/mL, continue to be put in CO
2incubator is cultivated 4h, then suck 100 μ L supernatants along culture fluid top, add 100 μ L DMSO, 10min is placed in dark place, utilize microplate reader (Sunrise company product) to measure light absorption value (wavelength 570nm), and calculating the cell survival situation according to light absorption value, 6 repeating holes are established in each processing.Cell survival rate (%)=Δ OD
drug treating/ Δ OD
blank* 100.
2. result: Incarviatone A has significant inhibitory action to the growth of application on human skin JEG-3 A431, HME1, A375 and SK23.This compound suppresses the IC of application on human skin JEG-3 A431, HME1, A375 and SK23 growth
50value is respectively: 1.23 ± 0.13 μ M, 2.24 ± 0.17 μ M, 1.21 ± 0.21 μ M and 2.10 ± 0.18 μ M.
By above-described embodiment, shown, Incarviatone A of the present invention has good inhibitory action to the growth of application on human skin JEG-3 A431, HME1, A375 and SK23.Prove thus, Incarviatone A of the present invention has anti-skin carcinoma activity, can be for the preparation of anti-skin carcinoma medicine.
Claims (1)
1.Incarviatone the application of A in treatment skin carcinoma medicine, described Compound I ncarviatone A structure as
formula Ishown in:
formula I.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201310432182.5A CN103446088B (en) | 2013-09-22 | 2013-09-22 | The application of Incarviatone A in preparation treatment skin carcinoma medicine |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201310432182.5A CN103446088B (en) | 2013-09-22 | 2013-09-22 | The application of Incarviatone A in preparation treatment skin carcinoma medicine |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN103446088A true CN103446088A (en) | 2013-12-18 |
| CN103446088B CN103446088B (en) | 2015-12-02 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201310432182.5A Expired - Fee Related CN103446088B (en) | 2013-09-22 | 2013-09-22 | The application of Incarviatone A in preparation treatment skin carcinoma medicine |
Country Status (1)
| Country | Link |
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| CN (1) | CN103446088B (en) |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2005021496A2 (en) * | 2003-08-27 | 2005-03-10 | The Trustees Of Columbia University In The City Of New York | Synthesis of derivatives of ginkgolide c |
| EP1939166A1 (en) * | 2006-12-19 | 2008-07-02 | InterMed Discovery GmbH | Plants extracts for use in brain modulation |
-
2013
- 2013-09-22 CN CN201310432182.5A patent/CN103446088B/en not_active Expired - Fee Related
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2005021496A2 (en) * | 2003-08-27 | 2005-03-10 | The Trustees Of Columbia University In The City Of New York | Synthesis of derivatives of ginkgolide c |
| EP1939166A1 (en) * | 2006-12-19 | 2008-07-02 | InterMed Discovery GmbH | Plants extracts for use in brain modulation |
Non-Patent Citations (1)
| Title |
|---|
| SHEN,Y.H.ET AL.,: "ncarviatone A,a structurally unique natural product hybrid with a new carbon skeleton from Incarvillea delavayi,and its absolute configuration via calculated electronic circular dichroic spectra", 《RSC ADVANCES2》, 31 December 2012 (2012-12-31), pages 4175 - 4180 * |
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| Publication number | Publication date |
|---|---|
| CN103446088B (en) | 2015-12-02 |
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| C41 | Transfer of patent application or patent right or utility model | ||
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Inventor after: Zhang Hongli Inventor before: Jiang Chunping Inventor before: Huang Rong |
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Effective date of registration: 20151103 Address after: 325011, building 1112, building A, 209 Wenchang Road, hi tech Zone, Longwan District, Zhejiang, Wenzhou Applicant after: Wenzhou Chengqiao Technology Co.,Ltd. Address before: Metro Technology Building No. 69 Olympic Avenue in Jianye District of Nanjing city in Jiangsu province 210019 01 5 storey buildings Applicant before: Nanjing Guangkangxie Biomedical Technology Co., Ltd. |
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Effective date of registration: 20181219 Address after: 210000 No. 30 Central Road, Gulou District, Nanjing City, Jiangsu Province Patentee after: Liu Huan Address before: 325011 room 1112, building A, 209 Wenchang Road, hi tech Zone, Longwan District, Wenzhou, Zhejiang. Patentee before: Wenzhou Chengqiao Technology Co.,Ltd. |
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Effective date of registration: 20190401 Address after: 233090 Zhongchuang Space A-43, 1st Floor, Chuangchuang Space, No. 8 Roadway 2595, Donghai Avenue, Bengbu City, Anhui Province Patentee after: Bengbu Yongyuan Electronic Technology Co., Ltd. Address before: 210000 No. 30 Central Road, Gulou District, Nanjing City, Jiangsu Province Patentee before: Liu Huan |
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Effective date of registration: 20191211 Address after: 239000 room 1602 and 1604, 3 building, 82 business center, Huayuan Road, Chuzhou, Anhui. Patentee after: Anhui Bodhi biological medicine science and Technology Co Ltd Address before: 233090 Zhongchuang Space A-43, 1st Floor, Chuangchuang Space, No. 8 Roadway 2595, Donghai Avenue, Bengbu City, Anhui Province Patentee before: Bengbu Yongyuan Electronic Technology Co., Ltd. |
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Granted publication date: 20151202 Termination date: 20200922 |